CFTR Activator Compounds for Tear Secretion and Constipation Relief

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Solution Overview

Problem

There is a need for safe and effective treatments for constipation and dry eye disorders, as existing therapies like laxatives and over-the-counter remedies provide limited relief, and current medications for dry eye do not address all symptoms effectively.

Innovation Solution

Development of compounds that activate the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) to treat constipation, dry eye, and other disorders by increasing tear secretion and improving intestinal function, using specific chemical structures to enhance CFTR activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing laxatives and over-the-counter remedies are used to treat constipation, then some symptomatic relief is provided, but the efficacy is limited and unsatisfactory

Engineering Contradiction:
ImproveefficacyVSAvoidlimited relief
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by developing novel chemical compounds with specific molecular structures (formula I) that target CFTR chloride channels. These compounds represent a fundamental change in the chemical parameters and mechanism of action compared to existing laxatives, transitioning from general osmotic or stimulant effects to specific ion channel activation, thereby achieving superior and more reliable efficacy in treating constipation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses CFTR chloride channel activators as intermediary substances that mediate the therapeutic effect. These compounds act as intermediaries between the administered drug and the physiological response, specifically activating CFTR channels to increase chloride secretion, which in turn drives water and electrolyte secretion into the intestinal lumen, producing reliable laxative effects

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If topical cyclosporine is used to treat dry eye, then ocular surface inflammation is reduced, but not all symptoms are eliminated

Engineering Contradiction:
Improvesymptom reliefVSAvoidresidual symptoms
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and addresses the specific mechanism of tear secretion by targeting CFTR chloride channels in the lacrimal gland. Rather than relying on cyclosporine's anti-inflammatory action alone, this approach directly stimulates tear production through CFTR activation, eliminating the limitation of incomplete symptom relief by adding a secretagogue mechanism to the therapeutic strategy

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent applies universality by developing CFTR activators that can simultaneously address multiple dry eye symptoms through a single mechanism. The compounds not only increase tear quantity but also potentially improve tear quality and ocular surface health, providing comprehensive symptom relief that goes beyond what anti-inflammatory therapy alone can achieve

Inventive Principle:
Principle #6Universality (Multi-functionality)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compounds effectively activate CFTR, leading to improved tear secretion and intestinal function, providing relief for constipation and dry eye symptoms, and demonstrating potential benefits in treating cholestatic liver and pulmonary diseases.

Implementation Method 1

compounds that activate the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) to treat constipation, dry eye, and other disorders by increasing tear secretion and improving intestinal function

Methodology Applied
Scientific EffectCFTR channel activation:

Data Source

PatentUS20260103446A1CFTR regulators and methods of use thereof
Publication Date: 2026.04.16 RGT UNIV OF CALIFORNIA
  • US20260103446A1 patent drawing
  • US20260103446A1 patent drawing
  • US20260103446A1 patent drawing

AI summary

Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders, and other diseases and disorders.